87873-72-1Relevant academic research and scientific papers
Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists
Fotsch,Sonnenberg,Chen,Hale,Karbon,Norman
, p. 2344 - 2356 (2007/10/03)
1-((1R,2R)-2-Hydroxy-1-methyl-2-phenylethyl)-1-methyl-3-(4-phenoxyphenyl)urea (1) was identified as a hit from the screening of the neuropeptide Y5 (NPY5) receptor. This lead was optimized for in vitro potency by changing the stereochemistry, the phenylethyl segment, the urea portion, and the 4-phenoxyphenyl group on the molecule. Over 40 analogues of 1 were prepared to study the structure-activity relationship for this series. The most potent compounds in this class have IC50S less than 0.1 nM at the NPY5 receptor (e.g., 40f, 44a, and 47). To determine the functional activity for this series of compounds, selected analogues were tested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor. All urea analogues tested in the functional assay acted as antagonists (e.g., 1, 32, 40a, and 44e).
Herbicidally active methyl-substituted tetrahydro-2-pyrimidinone derivatives
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, (2008/06/13)
Methyl-substituted tetrahydro-2-pyrimidinone derivatives of the general formula STR1 in which each Ar, independently of each other, represents an aryl group which is optionally mono- or poly-substituted by substituent(s) selected from halogen, C1 to C6 alkyl, C1 to C6 alkoxy, C1 to C6 alkylthio, nitro, phenoxy and trifluoromethyl, and R1, R2 and R3 independently represent a hydrogen atom or a methyl group, provided that at least one of R1, R2 and R3 represents a methyl group, are new and find use as herbicides, in particular as selective herbicides which may be used on weeds in crops such as cotton and rice. The N,N'-diaryl-N-haloalkyl-ureas which are starting materials for the production of compounds of formula (I) are also new.
